Drug intelligence / Profile preview

leucovorin

Development stage
Approved
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous, Intramuscular
01

Overview

Leucovorin is a chemically reduced derivative of folic acid and acts as an active metabolite (folinic acid). It is classified as a folic acid analog and functions primarily to protect healthy cells from the toxic effects of methotrexate and other folic acid antagonists by bypassing the inhibition of dihydrofolate reductase. This allows nucleic acid synthesis to proceed even in the presence of methotrexate. Leucovorin is also used to enhance the efficacy of fluorouracil in colorectal cancer by stabilizing the binding of its active metabolite (5-FdUMP) to thymidylate synthetase. Additionally, it can be used for treating certain types of anemia caused by low levels of folic acid.

Brand names
WellcovorinLederle Leucovorin
Other names
leucovorin calcium
02

Targets

RFC1 (Reduced folate carrier type 1)SLC46A1 (Proton-coupled folate transporter)

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